The bioactivity of caffeine aqueous solutions (0.20-2.00 wt %) and caffeine oleate emulsions (20 vol % oil, 2.00 wt % surfactant, 0.04 wt % caffeine, 0.05 wt % oleic acid) was assessed against two biological models: Drosophila melanogaster and Hypothenemus hampei. The caffeine aqueous solutions showed no insecticidal activity, whereas caffeine oleate emulsions had high bioactivity against both D. melanogaster and H. hampei. By preparing the caffeine oleate emulsions with anionic surfactants (i.e., sodium lauryl sulfate, sodium laureate, and sodium oleate), we obtained a lethal time 50 (LT50) of 23 min. In the case of caffeine oleate emulsions prepared with nonionic surfactants (i.e., Tween 20 and Tween 80), a LT50 of approximately 17 min was observed. The high bioactivity of the caffeine oleate emulsion against H. hampei opens the possibility of using this insecticide formulation as an effective way to control this pest that greatly affects coffee plantations around the world.